A series of novel 1,2,4-triazole thioacetanilide derivatives has been designed, synthesized and evaluated for
their anti-HIV activities in MT-4 cells. Half of these compounds showed moderate to potent activities against wild-type
HIV-1 with an EC50 ranging from 38.0 μM to 4.08 µM. Among them, 2-(4-(2-fluorobenzyl)-5-isopropyl-4H-1,2,4-triazol-
3-ylthio)-N-(2-nitrophenyl)acetamide 7d was identified as the most promising compound (EC50 = 4.26 µM, SI = 49).
However, no compound was active against HIV-2. The preliminary structure-activity relationships among the newly synthesized
congeners are discussed.
Keywords: HIV-1, AIDS, NNRTIs, 1, 2, 4-triazole thioacetanilides, Anti-HIV-1 activity.
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